7-Azaindole-3-acetic acid derivatives: Potent and selective CRTh2 receptor antagonists
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- 作者：David A. S ; ham ; Claire Adcock ; Kamlesh Bala ; Lucy Barker ; Zarin Brown ; Gerald Dubois ; David Budd ; Brian Cox ; Robin A. Fairhurst ; Markus Furegati ; Catherine Leblanc ; Jodie Manini ; Rachael Profit ; John
- 关键词：CRTh2 ; Prostaglandin D2 ; Azaindole ; Eosinophils ; Allergic diseases
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：15 August 2009
- 年：2009
- 卷：19
- 期：16
- 页码：4794-4798
- 全文大小：996 K
文摘
High throughput screening identified a 7-azaindole-3-acetic acid scaffold as a novel CRTh2 receptor antagonist chemotype, which could be optimised to furnish a highly selective compound with good functional potency for inhibition of human eosinophil shape change in whole blood and oral bioavailability in the rat.